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一种从宽体金线蛭中纯化得到的新型凝血酶诱导血小板聚集的选择性抑制剂。

A novel selective inhibitor to thrombin-induced platelet aggregation purified from the leech Whitmania pigra.

作者信息

Liu Xuan, Wang Caihui, Ding Xue, Liu Xiaodong, Li Qian, Kong Yi

机构信息

School of Life Science & Technology, China Pharmaceutical University, 24 Tong Jia Street, Nanjing 210009, PR China.

School of Life Science & Technology, China Pharmaceutical University, 24 Tong Jia Street, Nanjing 210009, PR China; State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, PR China.

出版信息

Biochem Biophys Res Commun. 2016 Apr 22;473(1):349-354. doi: 10.1016/j.bbrc.2016.03.117. Epub 2016 Mar 26.

DOI:10.1016/j.bbrc.2016.03.117
PMID:27021679
Abstract

BACKGROUND/AIM: The dried whole body of the leech Whitmania pigra, a well-known traditional Chinese medicine, has been widely used to treat thrombus diseases for thousands of years. However, its bioactive constituents were reported rarely. The aim of our study was to investigate antithrombotic components of it.

METHODS

The antithrombotic peptide was purified using a combination of anion-exchange chromatography, ultrafiltration and reverse-phase HPLC. the sequence of the peptide was determined using MALDI-TOF-MS-MS. Anti-platelet aggregation activity in vitro was evaluated using a turbidimetric method, and antithrombotic effect in vivo was assessed in an arterio-venous shunt thrombosis model in rats.

RESULTS

A novel antithrombotic peptide named WP-30, with the sequence VISRTQSNVQAAWGQVGGHAADYSAVAIER, was isolated from the dried whole body of the leech W. pigra. WP-30 selectively inhibited thrombin-induced anti-platelet aggregation in vitro, and potently attenuated thrombus formation in rats in vivo.

CONCLUSIONS

Taken together, we found a novel peptide from leech bodies, and this peptide showed antiplatelet aggregation and antithrombotic effects.

摘要

背景/目的:蚂蟥(宽体金线蛭)干燥全体是一种著名的传统中药,数千年来一直被广泛用于治疗血栓疾病。然而,其生物活性成分的报道却很少。本研究的目的是探究其抗血栓成分。

方法

采用阴离子交换色谱、超滤和反相高效液相色谱相结合的方法纯化抗血栓肽。使用基质辅助激光解吸电离飞行时间串联质谱法测定该肽的序列。采用比浊法评估体外抗血小板聚集活性,并在大鼠动静脉分流血栓形成模型中评估体内抗血栓作用。

结果

从宽体金线蛭干燥全体中分离出一种名为WP - 30的新型抗血栓肽,其序列为VISRTQSNVQAAWGQVGGHAADYSAVAIER。WP - 30在体外选择性抑制凝血酶诱导的抗血小板聚集,并在体内有效减轻大鼠血栓形成。

结论

综上所述,我们从蚂蟥体内发现了一种新型肽,该肽具有抗血小板聚集和抗血栓作用。

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